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Temanogrel

Name: Temanogrel
Brand: TargetMol
SKU: T17033
Price: 44 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T17033Cas No. 887936-68-7

Alias APD791

Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).

Temanogrel

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Purity: 99.24%

Catalog No. T17033Alias APD791Cas No. 887936-68-7

Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$44	In Stock	In Stock
5 mg	$111	In Stock	In Stock
10 mg	$165	In Stock	In Stock
25 mg	$277	In Stock	In Stock
50 mg	$393	In Stock	In Stock
100 mg	$533	In Stock	In Stock
200 mg	$691	-	In Stock
1 mL x 10 mM (in DMSO)	$121	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.24%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
Targets&IC50	5-HT2A:4.9 nM (ki)
In vitro	Temanogrel inhibits inositol phosphate accumulation (IC50: 5.2 nM). Temanogrel shows effective inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis (IC50: 13±7 nM) [1][3].
In vivo	Plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6, and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h, and 2.25 h after the start of treatment in dogs assigned to receive Temanogrel. There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment [3].
Synonyms	APD791

Chemical Properties

Molecular Weight	436.5
Formula	C₂₄H₂₈N₄O₄
Cas No.	887936-68-7
Smiles	COc1cccc(c1)C(=O)Nc1ccc(OCCN2CCOCC2)c(c1)-c1ccnn1C
Relative Density.	1.24 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (286.37 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.45 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2910 mL	11.4548 mL	22.9095 mL	114.5475 mL
5 mM	0.4582 mL	2.2910 mL	4.5819 mL	22.9095 mL
10 mM	0.2291 mL	1.1455 mL	2.2910 mL	11.4548 mL
20 mM	0.1145 mL	0.5727 mL	1.1455 mL	5.7274 mL
50 mM	0.0458 mL	0.2291 mL	0.4582 mL	2.2910 mL
100 mM	0.0229 mL	0.1145 mL	0.2291 mL	1.1455 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc